Table 2.
Receptor | Ligand | Ki (mean ± SEM) (nmol/L) | % Displacement | |
---|---|---|---|---|
dre-μ | Met-ENK | 684 ± 15 | 73.97 ± 1.29 | |
Leu-ENK | 1,317 ± 166 | 58.51 ± 2.68 | ||
β-END | 186 ± 25 | 88.45 ± 2.03 | ||
MEGY | 204 ± 53 | 78.98 ± 3.73 | ||
(d-Ala2)-MEGY | 744 ± 27 | 66.72 ± 0.81 | ||
(d-Ala2, Val5)-MEGY | 3,645 ± 621 | 43.16 ± 3.39 | ||
Morphine | 187 ± 94 | 100 | ||
Naloxone | 10.65 ± 1.53 | 100 | ||
| ||||
Ki (nmol/L) | Reference | |||
| ||||
dre-δ1 | β-END | 36.6 | 29 | |
MEGY | 427 | 21 | ||
Morphine | 22 | 29 | ||
dre-δ2 | Met-ENK | 45 | 30 | |
Leu-ENK | 175 | |||
MEGY | 146 | 21 | ||
Morphine | 1,400 | 30 | ||
rn-μa | Met-ENK | 1.80 | 5 | |
Leu-ENK | 6.19 | |||
MERF | 0.37 | |||
Morphine | 7.48 | |||
rn-δb | Met-ENK | 0.45 | ||
Leu-ENK | 0.37 | |||
MERF | 0.57 | |||
Morphine | 302 | |||
tg-μc | Met-ENK | 70.7 | 32 | |
Leu-ENK | 117 | |||
β-END | 55.9 | |||
tg-δc | Met-ENK | 24.9 | ||
Leu-ENK | 198 | |||
β-END | 284 |
This table summarizes the results obtained in competition binding assays (Ki and % displacement) using [3H]-diprenorphine on membrane homogenates from HEK293 cells that stably express the μ opioid receptor from zebrafish. The results of other competition binding studies for the zebrafish δ opioid receptors dre-δ1 and dre-δ2, prototypical mammalian δ and μ receptors rn-oprm1 (rn, Rattus norvegicus [rat]) and rn-oprm1 and the amphibian μ and δ receptors tg-oprm1 and tg-oprd1 (tg, Taricha granulosa [newt]) have also been included for comparison.
In this case, the radioligand used was the μ-selective peptidic analog [3H]-DAMGO and not [3H]-diprenorphine.
In this case, the radioligand used was the δ-selective peptidic analog [3H]-DPDPE and not [3H]-diprenorphine.
In this case, the radioligand used was the nonspecific antagonist [3H]-naloxone and not [3H]-diprenorphine.